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Antiproliferative Activity of (-)-Rabdosiin Isolated from Ocimum sanctum L.

Background: Ocimum sanctum L. (holy basil; Tulsi in Hindi) is an important medicinal plant, traditionally used in India. Methods: The phytochemical study of the nonpolar (dichloromethane 100%) and polar (methanol:water; 7:3) extracts yielded fourteen compounds. Compounds 6 , 7 , 9 , 11 , 12 , and 13 , along with the methanol:water extract were evaluated for their cytotoxicity against the human cancer cell lines MCF-7, SKBR3, and HCT-116, and normal peripheral blood mononuclear cells (PBMCs). Results: Five terpenoids, namely, ursolic acid ( 1 ), oleanolic acid ( 2 ), betulinic acid ( 3 ), stigmasterol ( 4 ), and β -caryophyllene oxide ( 5 ); two lignans, i.e., (-)-rabdosiin ( 6 ) and shimobashiric acid C ( 7 ); three flavonoids, luteolin ( 8 ), its 7- O - β -D-glucuronide ( 9 ), apigenin 7- O - β -D-glucuronide ( 10 ); and four phenolics, ( E) -p-coumaroyl 4- O - β -D-glucoside ( 11 ), 3-(3,4-dihydroxyphenyl) lactic acid ( 12 ), protocatechuic acid ( 13 ), and vanillic acid ( 14 ) were isolated. Compound 6 was the most cytotoxic against the human cancer lines assessed and showed very low cytotoxicity against PBMCs. Conclusions: Based on these results, the structure of compound 6 shows some promise as a selective anticancer drug scaffold.

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